Quantitative targeted absolute proteomics (QTAP)-based rational research on the human blood-brain barrier transport

Abstract

Quantitative targeted absolute proteomics (QTAP) has provided a rational strategy to determine the protein expression amounts of transporters which are involved in the highly regulated drug transport across the blood-brain barrier(BBB). This enables us to clarify the functional differences in the BBB transport between in vitro and in vivo, human and experimental animals such as monkeys and rodents, normal and disease conditions. The reconstruction of in vivo BBB transport function has been achieved by integrating the absolute amount of transporter proteins and the in vitro intrinsic transport activity for individual transporter, leading to the appropriate prediction of the human BBB central nervous system-acting drug transport.